- Synthetic method for antidepressant NSI189 and phosphate thereof
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The invention discloses a synthetic method for an antidepressant NSI189 and phosphate thereof. The method includes firstly activating 2-chloronicotinic acid A1 adopted as an initial raw material to obtain an acyl chloride compound; then reacting with N-monoprotected substituted piperazine to generate an intermediate A2; after removing the protecting group, reacting the intermediate A2 with a benzyl halide to generate an intermediate A3; reacting benzylamine or a benzylamine derivative A4 having a substitute on the benzene ring with isovaleraldehyde A5 to prepare an intermediate A6; coupling the intermediate A3 and the intermediate A6 to generate an intermediate A7; removing benzyl or derivative of the intermediate A7 under the existence of an inorganic acid or an oxidation agent to generate a compound A8; salifying the compound A8 with concentrated phosphoric acid to form a compound A9. In the method, all steps are easy to operate, reaction reagents are cheap and easily available, theproduct yield is high, the production cost is low, and no flammable combustible hazardous reagent or production operation is adopted, so that the method is suitable for large-scale industrial production and the method has a wide production application prospect.
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- Synthesis of a neurostimulative piperazine
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The invention describes an improved synthesis for piperazine derivatized with nicotinic acid and a benzyl moiety. The product compounds are useful for treatment of neurological conditions.
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